Figure 5.

(a) Inhibition by ciglitazone, MCC-555 and MAFP of [³H]2-OG hydrolysis by rat brain cytosolic fractions and by recombinant human MGL. The enzyme sources were preincubated with test compounds for 10 min at room temperature followed by addition of 2 μM [³H]2-OG. Incubation was carried out at room temperature for 2 h with cytosol preparations and 1 h with recombinant human MGL preparations. Values shown are mean±s.e.m., n=3–6. (b and c) Inhibition by ciglitazone and MCC-555 of the specific binding of 0.4 nM [³H]CP-55,940 to rat brain CB₁ (b) and human recombinant CB₂ receptors. (c) Values shown are means±s.e.m., n=3. CB, cannabinoid; MAFP, methyl arachidonyl fluorophosphonate; MCC-555, 5-[[6-[(2-fluorophenyl)methoxy]-2-napthalenyl]methyl]-2,4-thiazolidinedione; MGL, monoacylglycerol lipase; 2-OG, 2-oleoylglycerol.